Galicaftor-ABBV-2222-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGalicaftorCat.No.:HY-111111CASNo.:1918143-53-9Synonyms:ABBV-2222;GLPG-2222分?式:C??H??F?NO?分?量:559.46作?靶點:CFTR作?通路:MembraneTransporter/IonChannel儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(89.37mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7874mL8.9372mL17.8744mL5mM0.3575mL1.7874mL3.5749mL10mM0.1787mL0.8937mL1.7874mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(4.47mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.47mM);ClearsolutionBIOLOGICALACTIVITY?物活性Galicaftor(ABBV-2222;GLPG-2222)?種有效的，具有?服活性的囊性纖維化跨膜電導調(diào)節(jié)劑(CFTR)校正劑，可?于囊性纖維化的研究。體外研究Galicaftor(ABBV-2222;GLPG-2222)exhibitspotentinvitrofunctionalactivityinprimarypatientcellsharboringF508del/F508delCFTR,withanEC50[2].體內(nèi)研究TheratpharmacokinetictestsareperformedonGalicaftor(ABBV-2222;GLPG-2222;1mg/kg,i.v.;1mg/kg,p.o.)toillustrateitspharmacokineticpropertiesinrats.TheT1/2is2.7hours(i.v.).Andforintragastricadministration,thebioavailability(%F)is74%[1].REFERENCES[1].XueqingWang,etal.Discoveryof4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoicAcid(ABBV/GLPG-2222),aPotentCysticFibrosisTransmembraneConductanceRegulator[2].AshvaniKSingh,etal.BiologicalCharacterizationofF508delCFTRProteinProcessingbytheCFTRCorrectorABBV-2222/GLPG2222.JPharmacolExpTher.2020Jan;372(1):107-118.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Te